JPH06157277A - Skin comsetic - Google Patents

Abstract

PURPOSE:To obtain a skin cosmetic capable of effectively preventing melanism of skin and excellent even in safety. CONSTITUTION:The skin cosmetic contains glabridin and an antiphlogistic and is capable of suppressing inflammation and melanogenesis and melanin pigmentation caused by external irritation of ultraviolet rays, etc., by synergic action of these essential ingredients.

Description

Detailed Description of the Invention

[0001]

INDUSTRIAL APPLICABILITY The present invention can suppress inflammation caused by external stimuli such as ultraviolet rays and the production or deposition of skin melanin, and prevent erythema (sunburn), skin blackening, spots, freckles and the like. It relates to skin cosmetics.

[0002]

2. Description of the Related Art In the final stage of the process of darkening the skin color, tyrosine, which is one of the amino acids, produces the black pigment melanin by the action of tyrosinase. Therefore, it has been conventionally attempted to prevent pigment deposition by applying various agents having an action of inhibiting the action of tyrosinase, such as glutathione, vitamin C or its derivatives, to the skin. However, these drugs are not always satisfactory in terms of stability and effectiveness in topical application.

In addition to tyrosinase, this is a cause or a trigger for promoting the production of melanin, for example, activation of melanocytes by ultraviolet rays, involvement of various chemical mediators due to inflammation, involvement of active oxygen species produced by ultraviolet rays, and This is because it is difficult to sufficiently prevent the deposition of melanin even if a drug that merely inhibits the action of tyrosinase is applied, as reported by the involvement of sebum peroxide and the like.

[0004]

DISCLOSURE OF THE INVENTION The object of the present invention is to effectively prevent skin blackening, which is associated with many factors as described above, and is also excellent in safety. To provide new skin cosmetics.

[0005]

The skin cosmetic according to the present invention is characterized by containing glabridin and an anti-inflammatory agent as essential active ingredients, and is produced by external stimuli such as ultraviolet rays due to the synergistic action of these essential ingredients. It suppresses inflammation and skin melanin production and deposition. Glabridin, which is one of the active ingredients constituting the skin cosmetic of the present invention, is a compound having the structural formula of the following chemical formula 1, and is naturally a kind of licorice, Glycyrrhizaglabra Linne var. Turkish liquorice) contained in trace amount.

[0006]

[Chemical 1]

It has been confirmed that glabridin has a pharmacological action such as an antibacterial action, an antioxidative action, an anticarious action and an antiplasmin action, and it is also known that it has a melanin production inhibiting action (Japanese Patent Laid-Open No. Hei 10 (1999) -29242) 1-3110
11 publication). However, the previously confirmed melanin production inhibitory effect of glabridine is only when glabridine is used alone, and the effect when it is used in combination with an anti-inflammatory agent or other physiologically active substance has not been known.

When glabridin is extracted from licorice to be used as a raw material for producing cosmetics of the present invention, first, the root portion of licorice or its water extraction residue (for example, the residue obtained by extracting glycyrrhizin) is extracted with an organic solvent. As the extraction solvent, lower aliphatic alcohols such as methanol and ethanol; lower aliphatic ketones such as acetone; ethers such as dioxane and ethyl ether; halogenated hydrocarbons such as methylene chloride and chloroform; ethyl acetate, propyl acetate, etc. Esters such as butyl acetate; hydrocarbons such as hexane and benzene; and mixtures of two or more of these organic solvents can be used.

The licorice to be extracted is dipped in about 5 to 15 times the amount of the above solvent, and allowed to stand at room temperature or heated under reflux.
The extract obtained by distilling the solvent from the extract is usually 5 to
Although it contains about 10% of glabridin and can be used as it is in the cosmetic of the present invention, the use of a purified and highly purified cosmetic produces a cosmetic with more excellent use effect and less coloring. Obtainable. Purification
For example, it can be carried out by a method in which it is treated by normal phase silica gel chromatography and reverse phase chromatography and then crystallized from acetone. According to this method, a pure product of glabridin can be obtained relatively easily. In addition, the purification can be performed by employing any organic compound purification means such as column chromatography using a synthetic adsorbent or liquid-liquid countercurrent extraction.

The anti-inflammatory agent contained in the skin cosmetic of the present invention together with glabridin is an Adjubant arthritis inhibitory action, hyaluronidase inhibitory action, 5-lipoxygenase inhibitory action, plasmin inhibitory action, urokinase inhibitory action, vascular permeability inhibitory against carrageenin edema in rats. Action, anti-inflammatory action such as granulation growth inhibitory action or anti-allergic action
Any substance that has been confirmed by in vitro or in vivo pharmacological tests can be used. Specific examples of anti-inflammatory agents that can be used include allantoin, guaiaazulene, glycyrrhizic acid (or its water-soluble salts or derivatives), glycyrrhetinic acid (or its derivatives); stearyl epsilon aminocaproic acid; kamaazulene; zinc oxide; arnica extract, inchinko Extract, Scutellaria extract, Opacific extract, Chamomile extract, Licorice extract (water extract), Sanshishi extract, Sikon extract, Peony extract, Deer yak extract, Birch extract, Western horse mackerel extract, Tow There are plant extracts such as calendula extract, mukuroji extract, rosemary extract, yarrow extract, adzuki bean extract, senkyu extract and mugwort extract. Two or more kinds of these anti-inflammatory agents may be contained in the cosmetic of the present invention.

The suitable amount of glabridin in the skin cosmetic of the present invention varies depending on the kind of the cosmetic, but it is usually about 0.001 to 10% by weight, particularly preferably about 0.01 to 1.0. % By weight. The suitable amount of the anti-inflammatory agent is about 0.01 to 10% by weight, particularly preferably about 0.05 to 5% by weight, and further about 20 to 5000% by weight based on glabridin. It is desirable to mix it with. It goes without saying that when the anti-inflammatory agent is a plant extract having a coloring or a peculiar odor, it is desirable to add it within a range that does not adversely affect the appearance and the feeling of use of the cosmetic composition.

The cosmetics of the present invention include any cosmetics which can advantageously utilize the melanin production inhibitory action by the combined use of glabridin and an anti-inflammatory agent, such as lotions, emulsions, creams, packs, soaps and body shampoos. It can take the form. Cosmetic components other than glabridine and anti-inflammatory agents, such as oils and fats, surfactants, thickeners, pigments,
The fragrance, preservative, ethanol, polyhydric alcohol and the like can be arbitrarily selected depending on the type of the cosmetic, as long as the action of the two essential components is not impaired.

[0013]

Example [Preparation example of glabridin] 500 g of finely sliced licorice root was immersed in 5 liters of ethyl acetate and heated under reflux for 2 hours to extract the ethyl acetate-soluble component. The same operation was repeated for the extraction residue obtained by separating the extract, and a total of 9 liters of extract was obtained. The solvent of the extract was distilled off under reduced pressure to obtain 13.1 g of an extract containing glabridin. The extract was then dissolved in chloroform, sprinkled on silica gel and dried. The dried product was layered and packed on a column previously packed with 1 kg of silica gel (Wakogel C-300, manufactured by Wako Pure Chemical Industries, Ltd.), and eluted with a chloroform / methanol mixture (30: 1) to obtain a glabridin-containing fraction. Was collected. The solvent of this fraction was distilled off under reduced pressure to obtain 5.8 g of a solid substance, which was then dissolved in a small amount of methanol, sprinkled with reverse phase silica gel (ODSG-3, product of Mito Chemical Research Laboratory) and dried. , Reverse-phase silica gel 80 in advance
It was stacked and packed on a column packed with 0 g. A water / acetonitrile mixture (30/7
0) was passed and the fraction containing glabridin was collected. The solvent was distilled off from this fraction under reduced pressure to obtain a solid (4.3
g) was dissolved in 40 ml of acetone and allowed to stand at 5 ° C. for 3 days to obtain 3.8 g of crystals of glabridin. In each of the following examples, crystals of the above purified glabridin were used as glabridin.

Example 1 A whitening lotion was produced according to the formulation shown in Table 1. in this case,
First, the glabridin crystals of the above production example were dissolved in an ethanol / 1,3-butylene glycol mixed solution, and a surfactant (polyoxysorbitan monolaurate; 20E) was added.
O), fragrance and paraoxybenzoic acid ester were added and dissolved, then purified water and other components were added, and the mixture was stirred to homogenize.

[0015]

[Table 1] Lotion formulation (unit:% by weight) Note 1: The four kinds of plant extracts used as anti-inflammatory agents were obtained by adding 50% by weight of 1.3-butylene glycol to the crude material of each plant raw material, leaving it at room temperature for 7 days with occasional stirring, and then clarifying it. It is the extracted extract. ) Note 2: Formula 6 is a comparative example

Next, the use effect of each of the above lotions was tested by the following method. Test method: The back of a brown guinea pig was shaved, 0.1% oxoralen was applied thereto, and UVA 1 J / cm ² was irradiated after 30 minutes. One week later, for each site where pigment deposition was observed, 4 sections of 2 cm × 2 cm size were determined, and in each section, A: the above lotion as it was B: makeup without prescription 1 to 5 of glabridin Water C: Toner lotion from which the anti-inflammatory agent was removed from the above-mentioned lotion formulations 1 to 5 D: Any one of the lotion from which both glabridine and the anti-inflammatory agent were removed from the above-mentioned lotion formulations 1 to 5 times each morning and evening Apply continuously for 10 days, 2
The effect of suppressing erythema after 4 hours and the effect of suppressing pigmentation after 10 days were evaluated by visual observation (the color of the skin not treated with PUVA was used as a reference color).

The results are shown in Tables 2 and 3. Comparing the case of applying lotion containing both glaburidine and antiphlogistic to the example of application of lotion excluding glabridin or antiphlogistic, the former has the effect of suppressing erythema due to ultraviolet rays and the effect of suppressing pigmentation. Turns out to be better. In addition, no inflammation or other skin disorders were observed.

[0018]

[Table 2] Basic lotion formulation Erythema-suppressing effect Formulation 1 PUVA-untreated skin = A >> C = B >> D Formulation 2 PUVA-untreated skin = A >> C >> B >> D Formulation 3 PUVA-untreated skin = A >> C≥ B >> D Prescription 4 skin not treated with PUVA = A >> C = B >> D Prescription 5 skin not treated with PUVA = A >> C = B >> D

[0019]

[Table 3] Basic lotion formulation Pigmentation inhibiting effect Formulation 1 PUVA-untreated skin = A >>C> B ≧ D Formulation 2 PUVA-untreated skin ≧ A >>C> B = D Formulation 3 PUVA-untreated skin ≧ A >> C > B = D Prescription 4 Skin not treated with PUVA = A >>C> B = D Prescription 5 Skin not treated with PUVA = A >>C> B ≧ D

Example 2 A cream was produced according to the formulation shown in Table 4. At the time of production, the raw materials in the same table group were first melted at 70 ° C., mixed with the raw materials, and then heated to 78 ° C. Next, this was gradually added to the raw material heated to 75 ° C. with stirring to carry out preliminary emulsification. After that, apply a homogenizer to completely emulsify,
After cooling to 50 ° C, was added and cooled to 30 ° C. In addition, the prescription 11 is a comparative example.

[0021]

[Table 4] Cream prescription (unit:% by weight) (Note) Surfactant A: Self-emulsifying glycerin monostearate Surfactant B: Sorbitan monostearate Carboxyvinyl polymer: 1% aqueous solution

Next, the effect of use of each of the above creams was tested by the following method. Test method: The back of the brown guinea pig was shaved, and the shaved area was a 2 cm x 2 cm section 4.
It was divided into compartments and irradiated with UVB at 1 J / cm ² per day for 2 days. Since pigment deposition was observed after 4 days, A: the above cream as it was in each compartment B: a cream obtained by removing only glabridin from the above cream formulation C: a cream obtained by removing the anti-inflammatory agent from the above cream formulation D: formulation 11 Apply any one of the creams mentioned above once a day for 10 consecutive days.
The effect of suppressing pigmentation after day and the effect of suppressing erythema after 24 hours were determined by visual observation (using the color of the skin not subjected to UVB treatment as a reference color).

The results are shown in Tables 5 and 6. Comparing the case of applying cream containing glabridine and anti-inflammatory agent with the application example of cream excluding glabridine or anti-inflammatory agent, the former is superior in both erythema suppressing effect and pigmentation suppressing effect by UV rays to the latter. I understood. In addition, no inflammation or other skin disorders were observed.

[0024]

[Table 5] Cream basic formulation Pigmentation suppressing effect Formulation 7 UVB-untreated skin = A >>C> B = D Formulation 8 UVB-untreated skin ≧ A >>C> B = D Formulation 9 UVB-untreated skin = A >>C> B ≧ D Formula 10 UVB untreated skin = A >>C> B = D

[0025]

[Table 6] Cream basic formulation Erythema-suppressing effect Formulation 7 UVB-untreated skin ≧ A >> C ≧ B >> D Formulation 8 UVB-untreated skin ≧ A >> C ≧ B >> D Formulation 9 UVB-untreated skin ≧ A >> C ≧ B >> D Prescription 10 UVB untreated skin ≥A >> C ≥B >> D

[0026]

As described above, the cosmetic composition of the present invention containing glabridin and an anti-inflammatory agent can effectively prevent skin irritation and pigmentation due to ultraviolet rays, and no undesirable side effects are observed.

Claims (1)

[Claims] 1. A skin cosmetic, which comprises glabridin and an anti-inflammatory agent as essential components.